Ercan Z S, Türker R K
Pharmacology. 1977;15(2):118-26. doi: 10.1159/000136671.
The effects of histamine and 4-methylhistamine (a selective H2-agonist) were studied on the isolated rat stomach fundus and rabbit aortic strips superfused with Krebs' solution. The contraction induced by histamine was found to be mediated via mepyramine-sensitive H1, while the relaxation induced by the amine through metiamide-sensitive H2-receptors in both smooth muscles. Prior addition of metiamide to the superfusion medium caused an apparent dose-related potentiation in the response to histamine on the aortic strip but not on the stomach fundus strip. The relaxation produced by histamine on the aortic strip demonstrated when the muscle was pretreated with mepyramine and contracted by angiotensin II or serotonin. Metiamide competitively inhibited the relaxation induced by histamine but not by papaverine in both smooth muscles. 4-Methylhistamine produced only a relaxation in the rat stomach fundus which could be competitively inhibited by metiamide. This analog had no agonistic property in the aortic strip. From these results it was concluded that histamine H1-and H2-receptors are present in both smooth muscles. The predominant contractile effect of histamine is mediated through H1-receptors and the relaxing effect of the amine through H2-receptors.
研究了组胺和4-甲基组胺（一种选择性H2激动剂）对用Krebs溶液灌流的离体大鼠胃底和兔主动脉条的作用。发现组胺诱导的收缩是通过对美吡拉敏敏感的H1介导的，而该胺在两种平滑肌中通过对甲硫咪特敏感的H2受体诱导舒张。在灌流介质中预先加入甲硫咪特会使主动脉条对组胺的反应出现明显的剂量相关增强，但对胃底条则无此现象。当用美吡拉敏预处理肌肉并由血管紧张素II或5-羟色胺使其收缩时，组胺在主动脉条上产生舒张作用。甲硫咪特在两种平滑肌中竞争性抑制组胺诱导的舒张，但不抑制罂粟碱诱导的舒张。4-甲基组胺仅在大鼠胃底产生舒张作用，该作用可被甲硫咪特竞争性抑制。这种类似物在主动脉条中无激动特性。从这些结果得出结论，组胺H1和H2受体存在于两种平滑肌中。组胺的主要收缩作用通过H1受体介导，而该胺的舒张作用通过H2受体介导。
